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Compound Detail

CHEMBL336915

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CSCC[C@H](NC(=O)c1ccc(CN(Cc2c[nH]cn2)Cc2c[nH]cn2)cc1-c1ccccc1C)C(=O)O

Basic Information

ChEMBL ID CHEMBL336915
Phase Preclinical
Structure Type MOL
InChI Key DNQNJLLRSCYHPU-SANMLTNESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

532.7
MW (Da)
4.25
ALogP
6
HBA
4
HBD
127.0
PSA (Ų)
0.20
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N6O3S
MW 532.67
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.79

Activity Summary

IC50 1 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein farnesyltransferase
CHEMBL2094108
IC50 8.23 8.23 5.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein farnesyltransferase IC50 = 5.9 nM 8.23 Inhibition of Trypanosoma brucei protein farnesyltransferase 14711313

Literature References

PubMed DOI Target Context # Activities
14711313 10.1021/jm030236o Protein farnesyltransferase 2
14711313 10.1021/jm030236o Trypanosoma brucei brucei 1
14711313 10.1021/jm030236o Trypanosoma brucei rhodesiense 1
14711313 10.1021/jm030236o NIH3T3 1

Data from ChEMBL 36 via Core Engine